Chill Out: An Examination of Sleep & Relaxation Supplements

It’s no secret…in this day and age, people need to chill out a bit. From the overuse of stimulants such as caffeine in a world consumed with high-power coffee and energy drinks, the prevalence of anxiety and poor sleep quality is a common issue. Defined as “an abnormal and overwhelming sense of apprehension and fear often marked by physical signs (such as tension, sweating, and increased pulse rate), by doubt concerning the reality and nature of the threat, and by self-doubt about one’s capacity to cope with it”, anxiety is no joke (1). There are a variety of both pharmaceutical as well as supplemental items for helping alleviate anxiety as well as address poor sleep as they often go hand in hand. The goal of this article is to examine the most common supplements in use today for easing anxiety and promoting increase sleep quality.

Known chemically as β-Phenyl-γ-aminobutyric acid, phenibut is a derivative of the common supplement GABA, and is mostly found in the HCL form when used in products. While it is very similar to GABA in structure, only differing by a phenyl structure, it varies greatly as it allows the GABA molecule to cross the blood-brain barrier and exert effects (2). Devised in the 1960’s in Soviet Russia, the primary purpose was to treat PTSD, anxiety, insomnia, and depression (3). Interestingly, phenibut isn’t approved for clinical anywhere in the world aside from Russia, and instead is sold as a dietary supplement and even then, the legality often is regarded as a gray area in some countries.

Regarding effects, phenibut has an array of research examined effects. The primary ones of interest being sedation at higher dosages, with small amounts resulting in deep, restful sleep and improved sleep patterns (2). Also serving the dual purpose of functioning as an anxiety suppressor, phenibut has been shown to have powerful anxiolytic effects and promote cognitive euphoria (4). Interestingly, there also appears to be a focus enhancing effect at low doses, but this is diminished as the dose is increased and the sedative effects prevail (5).

Unfortunately, there does appear to be quite a list of negative effects associated with phenibut. Research has indicated that phenibut can have rebound anxiety, after cessation of its use for a time period correlated to duration and dosage (3). One of the commonly reported issues associated with phenibut is residual sleepiness, meaning that following use for sleep induction, the morning after can have a ‘groggy’ effect for a few hours after waking. Phenibut has also had reported issues of dependency, although in the few reported cases, individuals were using excessively high dosages (10g+) for long periods of time. Smaller dosages have not been shown to cause dependency.

Phenibut has a wide dosage range, going from 250-1000mg/day with starting at the low end of the spectrum being recommended. The dose should ideally be taken later in the day and not split the doses as it has a fairly long half-life.

Kava

Also known as kava root or kava kava, this is an herb native to the Southern Pacific. It has been used in traditional medicine for its psychotropic, hypnotic and in many cases its anxiolytic effects, often consumed as a brewed beverage. The anxiolytic effects are quite impressive with the potency appearing to rival pharmaceutical products. There is debate as to the safety of kava in some circles, with parts coming from the root knowns as rhizomes being considered safer than that coming from the aerial parts such as the leaves (6).

There are four active compounds that cross the blood brain barrier and exert effects including kawain, dihydrokawain, yangonin and desmethoxyangonin and the effects appear to begin to appear after about an hour (7). There is high correlation data supporting kava’s effects in treating non-psychotic anxiety as well as increasing subjective well-being (8). There has also been a substantiated increase in cognitive performance associated with kava specifically with increasing visual memory and short-term memory retrieval (9). Secondary effects of kava due to its anxiety relief effects also include improved sleep quality and depressive symptoms (10) (11).

Lastly, it is important to note that kava, in particular, has been suspect to interaction with pharmaceuticals so care should be taken if using kava in conjunction with prescriptions. Kava is best taken in the extract form at 300mg/day, divided into three 100mg doses for treating anxiety and cognitive issues. If taken for sleep, it is best taken as one large, single dose.

Passionflower

Formally known as Passiflora incarnata, passionflower is another interesting supplement that has been used in practice for a long time period. Discovered in 16th century Peru, it was traditionally used as a mild sedative and later on as an anti-anxiety, sleep disorder, hyperactivity and menopause relief supplement. It has been demonstrated in research that passionflower can be considered an effective drug in the treatment of generalized anxiety disorder and has an added advantage over certain prescriptions as it achieves this effect without appearing to impact job performance (12). The other key benefit supported by research for passionflower supplementation is that of sleep induction and sleep quality improvement as evidenced in numerous studies (13).

There is variances in the recommended dosing of passionflower and is most commonly consumed via passionflower tea. When used in concentrated supplement form, it is generally used at 1-2,000mg/day.

Technically known as N-acetyl-5-methoxytryptamine, Melatonin is a naturally occurring peptide hormone and neurotransmitter that is secreted by the pineal gland in the brain. It is found naturally in a variety of foods and plants such as tomato, walnuts, strawberries, olive oil and unprocessed dairy milk (14). There are also several supplements that contain melatonin including but not limited to Periostracum cicadae, Babreum coscluea (Shiya Tea-Leaf), Phellodendron amurense (Huangbo), Coptis chinesis and Angelica sinesis(15). Interestingly, there appears to be a correlation of melatonin levels and dietary lifestyle as diets rich in plant-based products can influence circulating melatonin levels due to plants containing melatonin in physiologically relevant levels (16). Effects of melatonin are exerted through melatonin receptors directly and are named MT1 and MT2 and are G-protein coupled receptors (GPRCs) (17).

Melatonin has been supported by research to have several positive effects through supplemental use. It is primarily known for its efficacy at helping to alleviate insomnia and in fact is the reference drug for insomnia related purposes, and appears to be highly effective at 3mg or even lower concentrations when taken before sleep (18). Directly related is that melatonin has been shown to help improve sleep quality for those suffering from conditions such as tinnitus (19). Another potential benefit of supplementation is that it appears to have a positive effect in treating stomach ulcers with a protective effect against both aspirin and heliobacter pylori induced stomach ulceration (20). Finally, there is some potential for melatonin in having a significant protective effect on the life in cancer patients with solid tumors, though it should be noted that the protective effect does not reach ‘half risk’ (RR of 0.50) and there is a significant fluctuation into the range of quarter risk (21).

Melatonin used for the purpose of improving healthy sleep patterns is best to be started at a dosage of .5mg to assess tolerance and progress up to 3-5mg if needed. There is no support for melatonin effectiveness being dose-dependent, so taking more will not result in falling asleep faster, nor is there substantiated evidence for higher doses being more beneficial.

Valerian Root

Valerian Root known formally asValeriana officinalis is a plant that has been used in traditional medicine dating as far back as ancient Greece for sedative effects, as an anxiolytic tea and as a treatment for insomnia (22). The bioactive components of valerian root include over 150 chemical constituents and many of them are physiologically active. They consist mainly of pyridine alkaloids; some organic acids and terpenes and the main bioactive component is valerenic acid which his found in the essential oil of the root (23). It can be sold in a variety of forms including its roots, rhizomes (underground stems), and stolons (horizontal stems). Typically, dried roots are prepared as teas or tinctures, and dried plant materials and extracts are put into capsules or incorporated into tablets (24).

Valerian Root has been used for a variety of sleep disorders including insomnia in research studies. The consensus is that there isn’t enough scientific data to support valerian root’s efficacy in supporting improved sleep quality. This is based on the collective analysis that measurements of sleep quality showed no difference between people that supplemented valerian and people that supplemented a placebo, however many participants anecdotally reported that their sleep was better when supplementing valerian (25).

It is promising that valerian root while not showing significant improvements in sleep quality can possibly promote relaxation independent of sleep improvements as high doses of valerian root have been shown to cause mild sedation (26). While not appearing to have significant efficacy for supporting sleep on its own, valerian root does appear to have strong research supporting its role as a positive modulator of GABA receptors, acting in a concentration-dependent manner on a site different from the GABA binding site and enhancing GABA neurotransmission (27). This is significant as often valerian root is supplemented in a complementary manner to GABA which is one of the main sedative neurotransmitters (28).

Valerian root is best taken in a dosage of 300mg 2 to 3 times per day with meals. If taken before bed, 60 minutes prior to bedtime appears to be best.

Gamma-aminobutyric Acid (GABA) is a naturally occurring potent depressive neuroactive peptide and is synthesized directly from the excitatory neurotransmitter glutamate via glutamate decarboxylase (29). It appears to have minimal uptake into the brain tissue via systemic circulation, though it does appear to have a positive effect on growth hormone secretion, especially in conjunction with resistance training and can additionally exert positive effects in regard to reducing anxiety and promote a state of calmness (30).

GABA has been implicated in several sleep mechanisms including dreaming, REM sleep and the sleep/wake cycle (31). It is important to note research has indicated that supplemental GABA cannot cross the blood-brain barrier, and instead exerts sleep enhancement effects on the body via increased alpha waves and decreased beta waves (32). Other positive yet ongoing research findings indicate that GABA might affect brain protein synthesis, improve many brain functions such as memory and study capability, lower the blood pressure of spontaneously hypertensive rats and may also have a relaxation effect in humans (33). There are varied recommendations for dosage based on what the user is looking to achieve. For stress relief 250mg, two to three times a day is recommended while a more potent dosage of up to 650mg, two to three times per day is recommended.

L-Tryptophan is a naturally occurring amino acid that is necessary for normal growth in infants and proper nitrogen balance in adults. It considered a precursor for serotonin and melatonin in the human body and additionally as a potential precursor for Niacin, albeit inefficient (34). L-tryptophan can be obtained through the diet as it is present in most protein-based foods or dietary proteins with chocolate, oats, milk, yogurt, cottage cheese, red meat, eggs, fish and poultry having the highest amounts (35).

L-Tryptophan has shown mixed results with supplementation in research. In regard to mood and supplementation, one study recorded the plasma tryptophan and mood levels of 50 healthy women were compared after following a 3-week, protein-sparing 1000 kcal diet, with a final week of being randomly allocated to receive either dietary tryptophan or a placebo, ultimately showing that there was no change in mood (36). Another study conducted over an 8-year study showed no associations between tryptophan intake, reduced depression or improved mood (37). When it comes to tryptophan depletion and its effects on mood and depression, however, the results are consistent.

A prime example of this is that in a meta-analysis of studies from 1966 through 2006, tryptophan depletion showed decreased mood states in participants with major depressive disorders, with a family history of depressive disorders, or with major depressive disorders in remission (38). Lastly, it is important to note that there is a marked difference in effects as consuming purified tryptophan increases the serotonin level in the brain, whereas eating foods containing tryptophan does not (39). This is because the transport system that brings tryptophan across the blood–brain barrier also transports other amino acids which are contained in protein food sources, and high blood plasma levels of other large neutral amino acids prevent the plasma concentration of tryptophan from increasing brain concentration levels (40).

Perhaps the most widely varying of the supplements in this category, tryptophan dosage is dependent on weight, age, and personal tolerance. For general mood elevation and anxiety treatment, a dose of 2-6g per day is a good starting point. For sleep quality improvement, the dose is 1-2g per day, however the efficacy of sleep improvement remains in question.

5-Hydroxytryptophan (5-HTP), also known as oxitriptan is a naturally occurring amino acid precursor of serotonin. In the body, the amino acid tryptophan is converted into 5-HTP via the enzyme tryptophan hydroxylase and then 5-HTP is consequently converted into serotonin via the enzyme L-amino acid decarboxylase (41). Direct 5-HTP in supplemental form is derived from the plant source Griffonia Simplicifolia and appears that it can be absorbed sublingually and has been shown to be more effective than supplementing with tryptophan in hopes of it converting to 5-HTP (42). Also of note and a testament to 5-HTP’s reliability in increasing serotonin levels is that it is often used as a clinical test to judge the potency of other drugs that affect serotonin levels (43).

On a basic level, 5-HTP has been used to restore normal serotonin levels in those who suffer from low serotonin in conditions such as depression or high levels of inflammation as an underlying condition such as metabolic syndrome (44). Ingestion of supplemental 5-HTP also appears to help reduce food intake via a secondary to increased satiety from food intake. It has also been further noted that it appears to specifically reduce cravings for carbohydrates in particular as the sertonergic system plays a role in macronutrient selection (45).

The optimal dosage for 5 HTP is 300-500mg/day, taken in divided doses for purposes of anxiety and mood improvement overall. For purposes of reducing food intake, it is recommended that 5 HTP be taken with a meal to help increase satiety.

L-Theanine, known by the technical name r-glutamylethylamide is a nondietary amino acid derived primarily from the natural source of Camellia sinesis. The theanine content of these leaves is approximately 0.9-3.1% of the dry weight of the leaves and said to range from 25-60mg per 200mL serving of tea (2.5g of dried tea leaves) (62). It is structurally similar to glutamine and is known as a relaxation agent without sedation with the proposed mechanism being a reduced perception of stress and slight improvements in attention (63).

Regarded as a relaxation agent without sedation and appears to act via blocking the effects of glutamate in the brain as well as stimulating the production of the inhibitory, relaxing neurotransmitter GABA (64). There is also a marked increase in alpha waves in the frontal and occipital lobes of the brain (65) and has research support in reducing stress perception and improvements in attention (66). Interestingly, there also appears to be a protective measure from theanine supplementation when taken before stressful situations in preventing the elevation of stress hormones and oxidative damage (67). Also of interest is that theanine has been shown in studies to significantly improve nitric oxide production in endothelial cells (68). L-theanine is generally taken in the dosage of 100-200mg per day and is commonly paired with caffeine.

Conclusion

There’s a lot of stress in the world around us and there isn’t any slowing down in this day and age. With the supplements outlined above, we now have a more intimate understanding of some of the potential options we have for helping take that edge off without the use of pharmaceutical means. Trial and error is the best way of seeing what you respond to, and as always, start with the lower end of the dosing spectrum and work your way up.

Suppz Recommended Sleep & Relaxation Supplements

With the wide variety of supplements available for sleep and relaxation, our experience has been best when taking these products in a blend. For sleep, you can’t go wrong with Hi Tech Somatomax or Repp Sports Hyper Sleep. Both include potent dosages of Phenibut and other nootropic relaxation compounds. For relaxation, we like Anastasis LAX, a more mild relaxation supplement that can help you calm down without feeling the need to sleep.